T1452

TPCA-1

Name: TPCA-1
Brand: SIGMA
Price: 762 PLN

≥95% (HPLC), IκB kinase-2 (IKK-2) Inhibitor, powder

Synonim(y):

[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide

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1 MG

762,00 zł

5 MG

3050,00 zł

762,00 zł

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Informacje o tej pozycji

Wzór empiryczny (zapis Hilla):

C₁₂H₁₀FN₃O₂S

Numer CAS:

507475-17-4

Masa cząsteczkowa:

279.29

UNSPSC Code:

12352200

PubChem Substance ID:

329826675

NACRES:

NA.77

MDL number:

MFCD09037541

Assay:

≥95% (HPLC)

Form:

powder

Quality level:

100

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Nazwa produktu

TPCA-1, ≥95% (HPLC)

SMILES string

NC(=O)Nc1sc(cc1C(N)=O)-c2ccc(F)cc2

InChI key

SAYGKHKXGCPTLX-UHFFFAOYSA-N

InChI

1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18)

assay

≥95% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: 5 mg/mL, clear

originator

GlaxoSmithKline

storage temp.

2-8°C

Quality Level

100

Powiązane kategorie

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

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Ta pozycja	SML1481	SML2724	SML2782
Sigma-Aldrich T1452 TPCA-1	Sigma-Aldrich SML1481 FzM1	Sigma-Aldrich SML2724 CC2-49	Sigma-Aldrich SML2782 Br-PBTC
form powder	form powder	form powder	form powder
assay ≥95% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 5 mg/mL, clear	solubility DMSO: 20 mg/mL, clear	solubility DMSO: 2 mg/mL, clear	solubility DMSO: 2 mg/mL, clear
color white to light brown	color white to beige	color white to beige	color white to beige

Application

TPCA-1 has been used to study its cytotoxic effects in RPMI8226 and LP1 cell lines[1]. It has also been used as a culture media supplement for nuclear protein fractions extracted from human airway smooth muscle cells.

Biochem/physiol Actions

IKK-2 Inhibitor

TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC₅₀ = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Preparation Note

TPCA-1 is soluble in DMSO at a concentration that is greater than or equal to 10 mg/ml. It is insoluble in water.

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Klasa składowania

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves

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Certyfikaty analizy (CoA)

Lot/Batch Number

0000463008

0000158500

0000109522

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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation.

Patricia L Podolin et al.

The Journal of pharmacology and experimental therapeutics, 312(1), 373-381 (2004-08-19)

Demonstration that IkappaB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-kappaB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-alpha and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment

TNFα-YAP/p65-HK2 axis mediates breast cancer cell migration.

Y Gao et al.

Oncogenesis, 6(9), e383-e383 (2017-09-26)

Clinical and experimental evidence indicates that macrophages could promote solid-tumor progression and metastasis. However, the mechanisms underlying this process remain unclear. Here we show that yes-associated protein 1 (YAP1), a transcriptional regulator that controls tissue growth and regeneration, has an

Interleukin-1β Signaling in Dendritic Cells Induces Antiviral Interferon Responses.

Lauren D Aarreberg et al.

mBio, 9(2) (2018-03-22)

Induction of interferon beta (IFN-β), IFN-stimulated genes (ISGs), and inflammatory responses is critical for control of viral infection. We recently identified an essential linkage of stimulation of the inflammatory cytokine interleukin-1β (IL-1β) and induction of ISGs that function as host

The E3 ubiquitin ligases HOIP and cIAP1 are recruited to the TNFR2 signaling complex and mediate TNFR2-induced canonical NF-κB signaling.

Alice Borghi et al.

Biochemical pharmacology, 153, 292-298 (2018-01-30)

Tumor Necrosis Factor (TNF) is a proinflammatory cytokine that elicits its action by binding to two cell surface TNF receptors (TNFR), TNFR1 and TNFR2, which are expressed by many different cell types. Stimulation of TNFR1 activates canonical NF-κB signaling, leading

Inhibition of IGF-1 signalling enhances the apoptotic effect of AS602868, an IKK2 inhibitor, in multiple myeloma cell lines.

Ines Tagoug et al.

PloS one, 6(7), e22641-e22641 (2011-07-30)

Multiple myeloma (MM) is a B cell neoplasm characterized by bone marrow infiltration with malignant plasma cells. IGF-1 signalling has been explored as a therapeutic target in this disease. We analyzed the effect of the IKK2 inhibitor AS602868, in combination

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TPCA-1